Pharmacology of Sedative Drugs
Pharmacology of Sedative Drugs
Pharmacology of Sedative Drugs
Conscious Sedation
Drugs
– Amnesia Midazolam
– Analgesia Opiates / Ketamine
– Relaxation IV anesthetics/Not
Ketamine
– Consciousness Avoid anesthetics
ALL SEDATIVES
Can Do the Following:
MIDAZOLAM Initial dose: Onset: 1 ½-5 min. Reduce dose by 1/3 to FLUMAZENIL P- Elderly/debilitated
(Dormicum) 1mg. – 1/2 when used with (Anexate)
elderly/debilitated Peak: 10-15 min. other CNS depressing C- Hypersensitivity, acute
2.5mg. – healthy drugs or in the elderly narrow angle glaucoma
Anxiolytic adult Duration: 60-90 or debilitated.
Sedative Initial dose should min. Manufacturer
S- CNS / Resp. depression
Amnesic not exceed 2.5mgm. recommends not more
- Hypotension
Anti-convulsant Usual max: Metabolized: liver than 1.5 mgm over at
- Agitation
Average adult<60 least two minutes in
- N/V, hiccups
years: Excreted: kidney patients with
5mg. within 30 min. Recovery is dose decreased pulmonary
Elderly adult >60 dependent, usually reserves.
years: 3.5 mg within 1-2 hrs.
30 min.
IV Dose rate: 1mg.
over 1 min. Wait 2
min. after each
increment to fully
evaluate effects.
Maintain level with
25% of initial IV
dose.
DIAZEPAM Initial dose: 2mg. Onset: 1-5min. Administer into large FLUMAZENIL P- Elderly/debilitated
(Valium) Usual Maximum: vein (Anexate)
10-20mg. within 30 Peak: 2 min. C- Hypersensitivity
mins. Inject close to IV site -Narrow angle glaucoma
Sedative Elderly 5-15 mgm. Duration: 15-60 If additives in IV - Psychosis
Anxiolytic over 30 mins. min. solution, flush tubing
Anti-convulsant IV Dose Rate: 2mg. before and after
S- CNS / resp. depression
over 3-5 min. Wait Metabolized: liver administration.
- N/V
5-10 minutes to
- Hypotension
Fentanyl Initial Dose: Onset: 1-2 min. Reduce dose by 1/4 to 1/3 Naloxone P- Elderly/debilitated
25mcg.- when used with other (Narcan) - Bradyarrhythmias
elderly/debilitated Peak: 3-5 min. CNS depressing drugs or - Head injury
Analgesia 25-50 mcg. –healthy adult in the elderly or - Resp. disease
Sedative Duration: 30-60 min. debilitated.
Usual Maximum: Muscle rigidity from high
100-250 mcg. within 30 Metabolized: liver doses may prevent C-Hpersensitivity
min. adequate chest wall
Excreted: kidney expansion and
IV Dose Rate: respirations. This is S- CNS/resp. depression
Administer slowly. Wait reversed with - Hypotension
5 minutes to evaluate neuromuscular blockers - Muscle rigidity
effect. Maintain level but patient must be - Bradycardia
with 25-50% of initial IV artificially ventilated - N/V
dose. - Puritus
-Seizures
Morphine Initial Dose: Onset: 1 min. Reduce dose by 1/3 to 1/2 Naloxone P- Elderly/debilitated
2.5mg.-elderly/debilitated when given with other (Narcan) -Respiratory conditions
5-10 mg. –healthy adult Peak: 15 min. CNS depressing drugs or -- Seizure disorders
in the elderly or -Head injury
Analgesia Usual Maximum: Duration: 2-4 hrs. debilitated
Sedative 10 mg. within 30 min. C- Hypersensitivity
Metabolized: liver - Biliary colic
IV Dose Rate: S- CNS/resp. depression
Administer slowly. Wait Excreted: kidney - Hypotension
5 min. to evaluate effects - N/V
-Dizziness
Pethedine Initial dose: Onset: 1 min. Reduce dose by 1/3 to 1/2 Naloxone P- Elderly/debilitated
25mg.-elderly/debilitated when given with other (Narcan) - SVT
(Demerol) 50mg.-healthy adult Peak: 5-7 min. CNS depressing drugs or - Seizure disorders
in the elderly or - Respiratory conditions
Usual Maximum Duration: 2-4 hr. debilitated.
100mg. within 30 min.
Analgesia
Sedative
Metabolized: liver C- Hypersensitivity
IV Dose Rate: - MAO inhibitors past 14 days
Administer slowly. Wait Excreted: kidney
5 minutes to evaluate
effects S- CNS/resp. depression
- Hypotension
- N/V
Thiopental Initial dose: Onset: 1- 2 min Reduce dose to 1/3 to 1/2 - S- Hypotension, myocardial depression,
(Pentothal) 50 - 100 mg Peak: 4-8 min when given with other CNS and respiratory depression, nausea,
Usual maximum: CNS depressing drugs or vomiting, diarrhea, laryngospasm
3mg/kg Duration of Action: in the elderly or C- Respiratory conditions
General anaesthetic Incremental and 10 - 30 min debilitated. Porphyrias
agent maximum doses are P- Inactive, debilitated, and elderly may
reduced to 1/3- 1/2 in the Metabolized: liver be more susceptible to adverse effects.
elderly. Increased toxicity with other CNS
Excreted: kidney depressants
KETAMINE Initial dose: Onset: 30 sec. IV Antisecretory agent such as - S- Nystagmus,resp. depression,
0.2 - 1.0 mg/kg 3-4 min. IM atropine (.01mgm/kg) or hypersalivation, laryngospasm, non-
(Ketalar) scopalamine given prior purposeful movements, emesis,
Barbituates and Ketamine
Usual maximum: Duration: 5-10 min. HR,B/P, ICP
should not be injected using
2mg/kg. IV - “Emergence reaction”
General anaesthetic the same syringe.
agent 12-25 min. Not recommended outside - Unpleasant dreams/hallucinations
IM the OR. (most common in females>age 10)
Propofol Initial dose: Onset: 30 sec Reduce dose by 1/3 to 1/2 - S- Respiratory depression,
10 - 20mg incremental Duration of Action: when given with other CNS - HR,B/P
(Diprivan) depressing drugs or in the
doses every 5 minutes as 10 - 15 min P- Hx CV disease or hypotension
needed elderly or debilitated. - Active pulmonary infection or disease
Restricted to monitored
General anaesthetic Usual Maximum: - Concomitant use with narcotics
ICU/ED patients and/or use
agent 100mg. by anesthesia personnel - Hx of airway instability, tracheal
Anti-emetic surgery or stenosis
Anti-convulsant Give slow IV push to
avoid hypotension.
Drugs Used for Pediatric Sedation
DRUG Pediatric Dose ONSET SPECIAL REVERSAL PRECAUTIONS
CONSIDERATIONS AGENT CONTRAINDICATIONS
& SIDE EFFECTS
MIDAZOLAM No manufacturer Onset: 1 ½-5 min. Reduce dose by 1/3 to FLUMAZENIL P- Debilitated
(Dormicum) published Peak: 10-15 min. 1/2 when used with (Anexate)
recommendations Duration: 60-90 other CNS depressing C- Hypersensitivity, acute
min. drugs or in the narrow angle glaucoma
Anxiolytic Metabolized: debilitated.
Sedative liver Manufacturer S- CNS / Resp. depression
Amnesic Excreted: kidney recommends not more - Hypotension
Anti-convulsant Recovery is dose than 1.5 mgm over at - Agitation
dependent, usually least two minutes in - N/V, hiccups
1-2 hrs. patients with decreased
pulmonary reserves.
Morphine 0.05-0.1mg/kg slowly Onset: 1 min. Reduce dose by 1/3 to Naloxone P- Debilitated
1/2 when given with (Narcan) -Respiratory conditions
Peak: 15 min. other CNS depressing -- Seizure disorders
Analgesia drugs or in the -Head injury
Sedative Duration: 2-4 hrs. debilitated. -C- Hypersensitivity
-Biliary colic
Metabolized: liver -S- CNS/resp. depression
- Hypotension
Excreted: kidney - N/V
-Dizziness
Pethedine 1-2 mg/kg slowly Onset: 1 min. Reduce dose by 1/3 to Naloxone P- Debilitated
(Demerol) 1/2 when given with (Narcan) - SVT
Peak: 5-7 min. other CNS depressing - Seizure disorders
drugs or in the - Respiratory conditions
Analgesia Duration: 2-4 hr. debilitated.
C- Hypersensitivity
Sedative - MAO inhibitors past 14 days
Metabolized: liver
S- CNS/resp. depression
Excreted: kidney - Hypotension
- N/V
Thiopental Initial dose: Onset: 1- 2 min Reduce dose to 1/3 to 1/2 - S- Hypotension, myocardial depression,
(Pentothal) 50 - 100 mg Peak: 4-8 min when given with other CNS and respiratory depression, nausea,
Usual maximum: Duration of Action: CNS depressing drugs or vomiting, diarrhea, laryngospasm
3mg/kg 10 - 30 min in the inactive or
General anaesthetic Incremental and Metabolized: liver debilitated. C- Respiratory conditions
agent maximum doses are Excreted: kidney Porphyrias
reduced to 1/3- 1/2 in the Not recommended outside
elderly. the OR.
Propofol Initial dose: Onset: 30 sec Reduce dose by 1/3 to 1/2 - S- Respiratory depression,
10 - 20mg incremental when given with other CNS - HR,B/P
(Diprivan) depressing drugs or in the
doses every 5 minutes as Duration of Action:
inactive or debilitated.
needed 10 - 15 min P- Hx CV disease or hypotension
General anaesthetic - Active pulmonary infection or disease
Restricted to monitored
agent Usual Maximum: - Concomitant use with narcotics
ICU/ED patients and/or use
Anti-emetic 100mg. - Hx of airway instability, tracheal
by anesthesia personnel
Anti-convulsant surgery or stenosis
Give slow IV push to
avoid hypotension.
Reversal Agents for Drugs used for Adult and Pediatric Sedation
NALOXONE Reversal of 0.4mg. –2mg. IV 0.01mg/kg every 2-3 min. Can precipitate VT/VF in P - Cardiovascular disease
(Narcan) patients with CV disease
narcotics May repeat as needed in May repeat as needed. or receiving potentially
2-3 min. intervals PRN cardiotoxic drugs. C- Hypersensitivity
If does not produce desired - Narcotic dependency
Onset: 1-2 min. outcome a subsequent dose
of 0.1mg/kg may be
administered. S- N/V, sweating
- Tachycardia, hypertension
Alternate infusion at - Pulmonary edema
0.4mg/hour
FLUMAZENIL Reversal of Initial dose: No manufacturer published Can precipitate seizures in P - Resedation, monitor for
(Anexate) 0.2mgm. IV over 15 sec. recommendations those with seizures resedation, respiratory
benzodiazepine Wait 45 sec, additional controlled by depression for up to 120 min.
induced 0.2mg. doses at one benzodiazepines, with Resedation least likely in low
minute intervals until tricyclic depression dose sedation,
sedation maximum of 4 additional overdose & with high risk (eg < 10mg Versed)
doses have been given. for seizures.
• Hypersensitivity
• Acute narrow angle glaucoma
Adult Sedation
Diazepam (Valium):
• A Benzodiazepine.
• No manufacturer published
recommendations
• Hypersensitivity
• Acute narrow angle glaucoma
• Psychosis
Potency
• Midazolam > Diazepam = 1:4
• No manufacturer published
recommendations
• Hypersensitivity
Adult Sedation
Morphine:
• An Opioid.
• Initial Dose: 2.5-10 mg.
• Maximum: 10 mg in 30 min.
• How to administer: Evaluate Your Patient first insert
& secure IV Give The Initial Dose Slowly Wait 5
min to evaluate effects Give Incremental Dosing in
order to maintain sedation level with ¼- ½ of the initial
dose DO NOT EXCEED MAX DOSE.
• Hypersensitivity
• Biliary colic
Adult Sedation
Meperidine, Pethidine (Demerol):
• An Opioid.
• Initial Dose: 25-50 mg.
• Maximum: 100 mg in 30 min.
• How to administer: Evaluate Your Patient first insert
& secure IV Give The Initial Dose Slowly Wait 5
min to evaluate effects Give Incremental Dosing in
order to maintain sedation level with ⅓ - ½ of the initial
dose DO NOT EXCEED MAX DOSE.
• 1 - 2 mg/kg slowly
• Elderly
• Debilitated
• Respiratory Disorders
• Seizure disorders
• SVT
• CNS depression
• Resp. depression
• Hypersensitivity
• MAO inhibitors
• Hypotension
• N/V
Potency
Fentanyl > Morphine > Pethidine
In equivalent doses ..
0.1 mg/kg Morphine=
1mg/kg Pethidine=1µg/kg Fentanyl
Discussion Questions
Fentanyl is:
CHLORAL HYDRATE
The Gold Standard of the 50’s for
Immobility, Non-painful Conscious
Sedation
i.e. The Radiology Suite
Disadvantages
• High failure rate (30%)
• Paradoxical excitement
• Maximum: 1.5 – 2 gm
NALOXONE Reversal of 0.4mg. –2mg. IV 0.01mg/kg every 2-3 min. Can precipitate VT/VF in P - Cardiovascular disease
(Narcan) patients with CV disease
narcotics May repeat as needed in May repeat as needed. or receiving potentially
2-3 min. intervals PRN cardiotoxic drugs. C- Hypersensitivity
If does not produce desired - Narcotic dependency
Onset: 1-2 min. outcome a subsequent dose
of 0.1mg/kg may be
administered. S- N/V, sweating
- Tachycardia, hypertension
Alternate infusion at - Pulmonary edema
0.4mg/hour
FLUMAZENIL Reversal of Initial dose: No manufacturer published Can precipitate seizures in P - Resedation, monitor for
(Anexate) 0.2mg IV over 15 sec. recommendations those with seizures resedation, respiratory
benzodiazepine Wait 45 sec, additional controlled by depression for up to 120 min.
induced 0.2mg. doses at one benzodiazepines, with Resedation least likely in low
minute intervals until tricyclic depression dose sedation,
sedation maximum of 4 overdose & with high risk (eg < 10mg Versed)
additional doses have for seizures.
been given.
Onset: 1-2 min. C- Hypersensitivity
Maximum cumulative - Seizure disorders
dose is 1.0 mg. - Tricyclic antidepressant
Peak effect: 6-10 min. Repeat above in 20 min. overdose
High Risk people may if needed - Benzodiazepine dependency
be necessary to increase No more than 3 mg. in
interval between doses one hour.
to over one minute. S - Visual disturbances,
diaphoresis, seizures,
arrhythmias
Discussion Questions
1. Fentanyl
2. Midazolam
3. Meperidine (Demerol)
4. Morphine
The following should be considered when
administering naloxone: